Proton exchange reactions in isotope chemistry (I)

摘要

Direct HD exchange reactions were applied to the preparations of stable isotope-labeled TKI258 and two TKI258 metabolites. Each compound was made in one single HD exchange reaction with excellent isotope incorporation. The number of deuterium incorporation and deuterium distribution in the molecules was similar in all three compounds. Stable isotope-labeled TKI258 was also prepared from d8-methylpiperazine in a multistep synthesis.